Product Description: PROTAC FAK degrader 2 (Compound F2) is a PROTAC degrader for focal adhesion kinase (FAK), with DC50 of 27.72 and 60.1 nM, for total FAK and phosphorylated p-FAK. PROTAC FAK degrader 2 inhibits cell viability of cancer cells 4T1, MDA-MB-231, MDA-MB-468 and MDA-MB-435, with IC50s of 0.73-5.84 μM. PROTAC FAK degrader 2 reverses the multidrug resistance (MDR) through inhibition of AKT and ERK signaling pathway. PROTAC FAK degrader 2 exhibits antitumor efficacy in HCT/8 xenograft mouse model. (Pink: ligand for target protein Ifebemtinib (HY-122844); Black: linker (HY-Y0681); Blue: ligand for E3 ligase Thalidomide (HY-14658))[1]
Applications: Cancer-Kinase/protease
Formula: C46H45F4N9O8
References: [1]Xu MS, et al., A novel FAK-degrading PROTAC molecule exhibited both anti-tumor activities and efficient MDR reversal effects. Acta Pharmacol Sin. 2024 Jun 6.
Molecular Weight: 927.90
Research Area: Cancer
Target: FAK;PROTACs
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